The opioid epidemic in the United States continues to take the lives of many individuals, with overdoses continuing to rise every year. Naloxone is an opioid antagonist that is efficacious in temporarily reversing opi...The opioid epidemic in the United States continues to take the lives of many individuals, with overdoses continuing to rise every year. Naloxone is an opioid antagonist that is efficacious in temporarily reversing opioid overdoses. Pharmacists play an important role in the accessibility and education of naloxone in both the community and health system settings. Recent efforts, such as co-dispensing naloxone with opioid prescriptions, naloxone training programs, and approval of naloxone to be over-the-counter, have been implemented in hopes to better control the opioid epidemic. Despite the efforts to make naloxone more accessible, there are still some barriers to overcome such as lack of training, cost, stigma, and patient refusal. This review aims to explore the contributions pharmacists have made thus far and define the barriers that still have to be resolved.展开更多
Background: Controlled-release oxycodone/naloxone(OXN-CR) maintains the effect of opioid-induced analgesia through oxycodone while reducing the occurrence rate of opioid-induced constipation through naloxone. The pres...Background: Controlled-release oxycodone/naloxone(OXN-CR) maintains the effect of opioid-induced analgesia through oxycodone while reducing the occurrence rate of opioid-induced constipation through naloxone. The present study was designed to assess the non-inferiority of OXN-CR to controlled-release oxycodone(OX-CR) for the control of cancer-related pain in Korean patients.Methods: In this randomized, open-labeled, parallel-group, phase IV study, we enrolled patients aged 20 years or older with moderate to severe cancer-related pain [numeric rating scale(NRS) pain score ≥4] from seven Korean oncology/hematology centers. Patients in the intention-to-treat(ITT) population were randomized(1:1) to OXNCR or OX-CR groups. OXN-CR was administered starting at 20 mg/10 mg per day and up-titrated to a maximum of80 mg/40 mg per day for 4 weeks, and OX-CR was administered starting at 20 mg/day and up-titrated to a maximum of 80 mg/day for 4 weeks.The primary efficacy endpoint was the change in NRS pain score from baseline to week4, with non-inferiority margin of-1.5. Secondary endpoints included analgesic rescue medication intake, patientreported change in bowel habits, laxative intake, quality of life(QoL), and safety assessments.Results: Of the ITT population comprising 128 patients, 7 with missing primary efficacy data and 4 who violated the eligibility criteria were excluded from the efficacy analysis. At week 4, the mean change in NRS pain scores was not significantly different between the OXN-CR group(n = 58) and the OX-CR group(n = 59)(-1.586 vs.-1.559,P = 0.948). The lower limit of the one-sided 95% confidence interval(-0.776 to 0.830) for the difference exceeded the non-inferiority margin(P < 0.001). The OXN-CR and OX-CR groups did not differ significantly in terms of analgesic rescue medication intake, change in bowel habits, laxative intake, QoL, and safety assessments.Conclusions: OXN-CR was non-inferior to OX-CR in terms of pain reduction after 4 weeks of treatment and had a similar safety profile. Studies in larger populations of Korean patients with cancer-related pain are needed to further investigate the effectiveness of OXN-CR for long-term pain control and constipation alleviation.Trial registration ClinicalTrials.gov NCT01313780, registered March 8。展开更多
5-HT content in medulla oblongata plus pons and DA level in brain stem obviously increased,while NA concentration in telencephalon markedly decreased in EAA.A previous injection ofnaloxone,a blocker of opiate receptor...5-HT content in medulla oblongata plus pons and DA level in brain stem obviously increased,while NA concentration in telencephalon markedly decreased in EAA.A previous injection ofnaloxone,a blocker of opiate receptor,could partially inhibit the EAA,abolish the effects ofEA’s increasing the 5-HT content in the medulla oblongata plus pons and the DA level in thebrain stem,and decrease the NA level in the diencephalon after EA.These results indicate thatEA may mediate the metabolism of the central monoamine neurotransmitters partially via opiatereceptor to exert its analgesic effect.展开更多
Stimulating SmI cortex like needling points produced analgesic effect in rats.Under the background of ventrical microinjecting atropine（10μg/2μl）or naloxone（20μg/20μl）tailflick latency（TEL）remained unchanged...Stimulating SmI cortex like needling points produced analgesic effect in rats.Under the background of ventrical microinjecting atropine（10μg/2μl）or naloxone（20μg/20μl）tailflick latency（TEL）remained unchanged after stimulating SmI.Comparing atropine group or naloxone group with normal saline group it was shown that there were a statistical difference in TFL between the two groups respectively.Thus,both ACh and endogenous morphine-like factors may participate in analgesic effect as a neurotransmitter of the corticofugal modulation of pain.展开更多
Objective: To investigate the effects of naloxone hydrochloride on pulmonary function, blood gas changes and inflammatory factors in patients with COPD combined with respiratory failure. Methods: According to random d...Objective: To investigate the effects of naloxone hydrochloride on pulmonary function, blood gas changes and inflammatory factors in patients with COPD combined with respiratory failure. Methods: According to random data table method, 80 cases of COPD combined with respiratory failure were randomly divided into the control group (n=40) and observation group (n=40), patients in the control group were treated with noninvasive positive pressure ventilation on the basis of routine symptomatic treatment, on the basis of the treatment of the control group, the observation group received naloxone hydrochloride therapy. The levels of pulmonary function, blood gas changes and inflammatory factors were compared in two groups before and after treatment. Results: The levels of serum FEV1, FVC, PEF, PaCO2, PaO2, PaO2/FiO2, TNF-α and PCT in the two groups before treatment were not statistically significant. After treatment, the levels of FEV1, FVC, PEF in the control group and observation group were (70.01±0.36)%, (2.16±0.41) L, (2.98±0.45) L/s and (81.71±0.53)%, (3.65±0.55) L, (4.36±0.43) L/s, which were significantly higher than those in the same group before treatment, and the levels in observation group were significantly higher than those in the control group;the levels of PaCO2, PaO2 and PaO22/FiO2 in the two groups were (59.62±6.47) mmHg, (65.53±7.36) mmHg, (323.89±10.47) and (46.59±6.64) mmHg, (73.65±8.26) mmHg, (398.64±14.06), compared with the same group before treatment, PaCO2 levels were significantly lower in both groups, and the observation group was significantly lower than the control group, PaO2,PaO2/FiO2 levels were significantly increased in both groups, and the observation group was significantly higher than the control group;the levels of TNF-α, PCT in the two groups were (23.28±4.53) pg/mL, (5.22±2.13) ng/mL and (16.61±4.12) pg/mL, (2.07±1.21) ng/mL, which were significantly lower than those in the same group before treatment, moreover, the observation group levels were significantly lower than those in the control group. Conclusion:Treatment of COPD with respiratory failure by naloxone hydrochloride can effectively reduce the level of inflammatory factors, and improved lung function and blood gas levels, which has important clinical value.展开更多
Objective: To investigate the effect of Shenqi Fuzheng Injection combined with naloxone and BiPAP ventilator on serum inflammatory factors, immune function and blood gas analysis indexes in treatment of AECOPD with ty...Objective: To investigate the effect of Shenqi Fuzheng Injection combined with naloxone and BiPAP ventilator on serum inflammatory factors, immune function and blood gas analysis indexes in treatment of AECOPD with type Ⅱ respiratory failure. Methods: A total of 82 patients with AECOPD and type Ⅱ respiratory failure were divided into control group (n=40) and observation group (n=42) according to random data table, patients in the control group received naloxone and BiPAP ventilator therapy, and observation group patients were treated with Shenqi Fuzheng Injection on the basis of control group. The levels of serum inflammatory factors, immune function and blood gas analysis indexes were compared between the two groups before and after treatment. Results: There were no significant difference in levels of CRP, TNF-α, IL-6, CD3+, CD4+, CD8+, CD4+/CD8+, PaO2, PaCO2, SaO2 and pH before and after treatment in the two groups. After treatment, the levels of CRP, TNF-α, IL-6, CD8+and PaCO2 in two groups were significantly lower than those in same group before treatment, moreover observation group was significantly lower than control group;and levels of CRP, TNF-α, IL-6, CD8+ and PaCO2 in the observation group was significantly lower than those of the control group, the difference was statistically significant;When compared with the group before treatment, CD3+, CD4+, CD4+/CD8+, PaO2, SaO2 and pH levels of both groups after treatment were significantly increased, and the level of each index of observation group after treatment were significantly higher than the control group, the difference was statistically significant. Conclusion: The clinical effect of Shenqi Fuzheng Injection Combined with naloxone and BiPAP ventilator in treatment of AECOPD with type II respiratory failure is significant, can effectively reduce the body's inflammatory reaction, improve immune function, regulate blood gas analysis index, with a certain clinical value.展开更多
Objective This study aimed to investigate the effects of Montanide ISA-720 and Naloxone(NLX)in Hepatitis B surface antigen(HBsAg)vaccine formulation on cytokine and long-lasting antibody responses.Methods First,the HB...Objective This study aimed to investigate the effects of Montanide ISA-720 and Naloxone(NLX)in Hepatitis B surface antigen(HBsAg)vaccine formulation on cytokine and long-lasting antibody responses.Methods First,the HBsAg was formulated in Montanide ISA-720 adjuvant and Naloxone at 5 and 10mg/kg.The experimental mice were immunized three times at a 2-week interval,and then IL-4,IL-2,TNF-α,and IFN-γcytokines;long-lasting IgG antibody responses 220 days after the last shot;and IgG1/IgG2a isotypes were assessed by ELISA.Results The HBsAg-Alum group exhibited the highest IL-4 cytokine response among the experimental groups,whereas NLX in HBsAg-MON720 vaccine formulation did not affect cytokine responses.In addition,NLX in Alum-based vaccine suppressed IL-4 cytokine response and increased the IL-2/IL-4 cytokine ratio.Moreover,HBsAg-MON720 was more potent than HBsAg-Alum in the induction of antibody responses,and NLX in Alum-and MON720-based vaccines induced long-lasting antibody responses.Conclusion NLX in Alum-based vaccine decreased IL-4 cytokine response,increased IL-2/IL-4 cytokine ratio,and improved long-lasting humoral immune responses in both vaccine formulations.Therefore,the adjuvant activity of NLX in the vaccine formulation depends on the type of adjuvant and the nature of the antigen in the vaccine formulation.展开更多
Spinal cord injury(SCI)causes Ca^(2+) overload,which can lead to inflammation and neuronal apoptosis.In this study,we prepared a nanovesicle derived from macrophage membrane(MVs),which encapsulated sodium alginate(SA)...Spinal cord injury(SCI)causes Ca^(2+) overload,which can lead to inflammation and neuronal apoptosis.In this study,we prepared a nanovesicle derived from macrophage membrane(MVs),which encapsulated sodium alginate(SA)and naloxone(NAL)to inhibit inflammation and protect neurons by reducing the free Ca^(2+) concentration at the SCI site.Based on the transmission electron microscopy(TEM)image,the encapsulated sample(NAL–SA–MVs)had a particle size of approximately 134±11 nm and exhibited a sustained release effect.The encapsulation rate of NAL and SA was 82.07%±3.27%and 72.13%±2.61%in NAL–SA–MVs,respectively.Targeting tests showed that the NAL–SA–MVs could accumulate in large quantities and enhance the concentration of SA and NAL at the lesion sites.In vivo and in vitro studies indicated that the NAL–SA–MVs could decrease the concentration of free Ca^(2+),which should further alleviate the inflammatory response and neuronal apoptosis.Anti-inflammation results demonstrated that the NAL–SA–MVs could reduce the pro-inflammation factors(iNOS,TNF-α,IL-1β,IL-6)and increase the expression of antiinflammation factors(IL-10)at the cell and animal level.Concurrently,fluorescence,flow cytometry and western blot characterization showed that the apoptotic condition of the neurons was significantly inhibited.In addition,the motor function of C57 mice were significantly improved after NAL–SA–MVs treatment.In conclusion,it is suggested that the NAL–SA–MVs has tremendous potential in the treatment of SCI.展开更多
Experiments were performed on SD rats. The animals were anesthetized with urethane (1. 0 g/kg, i. p. ). The diaphragmatic electric activity and intratracheal pressure were monitored. Morphine (4 mg/kg, i. v. ) caused ...Experiments were performed on SD rats. The animals were anesthetized with urethane (1. 0 g/kg, i. p. ). The diaphragmatic electric activity and intratracheal pressure were monitored. Morphine (4 mg/kg, i. v. ) caused marked respiratory inhibition. The respiratory frequency (RF), integrated diaphragmatic electric activity (IDEA) and diaphragmatic minute activity (DMA) were decreased. The respiratory depression effect of morphine was almost completely eliminated by pretreatment with naloxone injected into the medial areas of the nucleus retrofacialis (mNRF). Bilateral microinjection of morphine (5 μg) into mNRF might result in apnea in all animals. This effect could be fully prevented by injection of naloxone into mNRF in advance. The results suggest that there might be morphine receptors in the mNRF and they might play an important role in the respiratory inhibition induced by systemic administration of morphine.展开更多
The recent large increase in deaths involving opioids (whether prescription or illicit, pure or adulterated, alone or in combination with other drugs) is the manifestation of a complex, and multifaceted problem consis...The recent large increase in deaths involving opioids (whether prescription or illicit, pure or adulterated, alone or in combination with other drugs) is the manifestation of a complex, and multifaceted problem consisting of psychological, psychosocial, medical, legal, regulatory, economic, cultural, and political components, among others. Because the problem involves issues related to both supply and demand, the solution is not obvious, simple, or quick. There is no easy fix. Preventing and treating opioid misuse and abuse requires a comprehensive, time-intensive, and expensive intervention supported by public policy and support through coordinated medical, regulatory, legal, and financial guidelines and practice. But until the long-term problems can be fixed, the immediate crisis of overdose deaths can be ameliorated by making available an opioid receptor antagonist to reverse the respiratory depression that is the cause of death to those who are in the best position to administer it in time (professionals, untrained bystanders, and even fellow drug abusers). The statistics overwhelmingly demonstrate that this is a life-saving medical intervention. Yet, there is still uncertainty about this intervention, and even some opposition to it. We describe the scientific basis for the approach and the issues surrounding its use to treat accidental or intentional overdose by pain patients, recreational opioid users, and addicts. We also describe the calls to limit the number of times it should be available to a user and the limitations of its effectiveness—mainly that it only addresses the acute death crisis, not the underlying problems that led to it.展开更多
The mechanism(s) of analgesic action of paracetamol (acetaminophen;N-acetyl-p-aminophenol) remains controversial. Previous studies on rats suggested that the antinociceptive action of paracetamol might involve the cen...The mechanism(s) of analgesic action of paracetamol (acetaminophen;N-acetyl-p-aminophenol) remains controversial. Previous studies on rats suggested that the antinociceptive action of paracetamol might involve the central descending inhibitory pain pathways recruiting both a serotoninergic and an opioidergic system. This study explores this issue in mice using paroxetine, the most potent selective serotonin re-uptake inhibitor, and the nonselective opioid pure antagonist naloxone. Animals were divided into two main groups for two separate experiments, each subdivided into 3 subgroups. In both experiments;the first group served as control, the second group received paracetamol (200 mg/kg, i.p). In one experiment, the third group received paroxetine (20 mg/kg p.o for 7 days) before paracetamol. In the other experiment, animals of the third group were pretreated with naloxone (5 mg/kg, i.p) 30 min before paracetamol. The antinociceptive effect of paracetamol was tested using the hot plate test. Paracetamol displayed a significant antinociceptive activity that was augmented by pretreatment with paroxetine as was shown by maintenance of its effect beyond that shown by paracetamol alone. On the other hand, pretreatment with naloxone abolished paracetamol’s antinociceptive activity in the hot-plate test. These results extended the previous observation in rats that the antinociceptive effect of paracetamol involved activation of a central descending pain inhibitory pathway with serotonin and opioidergic peptides being potential mediators recruited.展开更多
A 56-year-old man presented to the emergency department after an intentional overdose of oxycodone and ethanol.He was previously opioid-naive with no other medical history.He subsequently developed acute abdominal pai...A 56-year-old man presented to the emergency department after an intentional overdose of oxycodone and ethanol.He was previously opioid-naive with no other medical history.He subsequently developed acute abdominal pain with nausea and vomiting.A computed tomography scan of his abdomen and pelvis revealed distension of his stomach with no other abnormalities suggestive gastroparesis.He was subsequently treated with intravenous naloxone with complete resolution of his symptoms soon after.This case highlights the association between opioids and acute gastrointestinal mobility disorders contrary to the traditional association with chronic opioid use,as well as the utility of naloxone as a treatment.展开更多
Objectives:To investigate the effectiveness and safety of Xingnaojing Injection(XNJ,醒脑静注射液)compared with naloxone for the treatment of acute alcohol intoxication(AAI),and provide the latest evidence through evid...Objectives:To investigate the effectiveness and safety of Xingnaojing Injection(XNJ,醒脑静注射液)compared with naloxone for the treatment of acute alcohol intoxication(AAI),and provide the latest evidence through evidence-based approach.Methods:Seven electro-databases including Pub Med,EMBASE,Cochrane Central Register of Controlled Trials,Chinese National Knowledge Infrastructure Databases,Chinese Biomedical Literature Database,Chinese Science and Technology Periodical Database(VIP)and Wanfang Database were searched from the inception to January 2018.Randomized controlled trials(RCTs)comparing XNJ with naloxone for patients with AAI and reporting at least one of the below outcomes were included:patients’conscious recovery time,stay length in emergency department,disappearance time of the ataxia symptom,the severity of the symptoms,the blood alcohol content as wel as the adverse events.Methodological quality of included trials was assessed using the risk of bias tool which recommended by the Cochrane Col aboration.Meta-analysis was conducted by Review Manager 5.3 software.Results:Total y 141 trials with 13,901 patients were included in this review,al of them were assessed as unclear or high risk of bias.Results showed that on the basis of routine therapy,standard dose XNJ(10–20 m L)may have similar results with naloxone on the recovery time of consciousness(MD 12 min,95%CI 7.2–17.4 min)and disappearance time of symptoms(MD 6 min,95%CI–13.8–25.8 min)for patients with AAI.Larger dose of XNJ Injection(21–40 m L)may speed up the time(almost 1 h earlier).Combination of XNJ and naloxone seemed superior to the naloxone alone for al the relevant outcomes.The average difference of time in consciousness recovery was 2 h and the number of AAI patients whose consciousness recovery within 1 h was above 50%the combination group than in the control group(RR 1.42,95%CI 1.29 to 1.56).No severe adverse events or adverse reactions of XNJ were reported in the included trials.Conclusions:Low quality of evidence showed XNJ may have equal effect as naloxone and may achieve better effect as add-on intervention with naloxone for patients with AAI.We failed to evaluate the safety of XNJ Injection due to the insufficient evidence in this review.展开更多
It has been shown in our previous experiments that arcuate nucleus (ARC) stimulation had a marked analgesic effect. After selective lesion of ARC neurons by neonatally intrapcritoneal injection of monosodium glutamate...It has been shown in our previous experiments that arcuate nucleus (ARC) stimulation had a marked analgesic effect. After selective lesion of ARC neurons by neonatally intrapcritoneal injection of monosodium glutamate (MSG), the analgesic effects of morphine, acupuncture and stress decreased significantly.展开更多
BACKGROUND: Scorpion venom from Buthus martensii Karsch is a kind of protein toxin secreted by scorpion tail. According to records of Pen-ts’ao Kan-mu, the dried scorpion’s body and tail are used as medicine, which ...BACKGROUND: Scorpion venom from Buthus martensii Karsch is a kind of protein toxin secreted by scorpion tail. According to records of Pen-ts’ao Kan-mu, the dried scorpion’s body and tail are used as medicine, which mainly treating rheumatism numbness, pain and convulsion. Some researches consider that scorpion toxin is the main pharmacological active component of the dried scorpion, and it has 4 times stronger analgesic effect on somatic pain than morphine. OBJECTIVE: To observe the interventional effect of scorpion venom of Buthus martensii Karsch analgesic active peptide on somatic pain. DESIGN: A randomized and controlled trial. SETTING: Department of Physiology, Shenyang Medical College. MATERIALS: Totally 80 Wistar rats (provided by Animal Center of Shenyang Medical College), male and female in half, aged 3 to 4 months, weighed 250 to 350 g, were used in this trial. They were randomly divided into 4 groups: experimental group, control group, morphine group and naloxone group, with 20 in each group. Analgesia active peptide from buthus martensii karsch venom (provided by Biochemical Department of Shenyang Pharmaceutical University, 1 mL/dosage), morphine (produced by Shanghai First Pharmaceutical Manufacturing Plant), naloxone (opium acceptor inhibitor, American Sigma Corporation), ATAC-350 data-processing machine (Nihon Kohden Corporation), X-Y recording instrument (Nihon Kohden Corporation). METHODS: The experiment was conducted in the Department of Physiology, Shenyang Medical College from July 2003 to July 2005. ① After all the animals were anesthetized, common peroneal nerve is dissected and ligated at middle part. Posterior nucleus group of thalamus (PO) and the tail nuclear were oriented according to G. Paxino rat brain three-dimensional orientation atlas. Glass micro electrode was inserted into PO as guiding electrode, connected with ATAC-350 data-processing machine and X-Y recording instrument, to record the unit evoked potential of PO, taking the evoked potential discharge of the common peroneal nerve of PO as the somatic pain index.② Single square-wave stimulation of intensity 17-19 volt, wave wide 0.2 ms, time delay 20 ms was exerted on common peroneal nerve. The time interval was 5 minutes. X-Y recording instrument was used to draw the graph. 0.002 mg scorpion venom analgesic active peptide was injected into the rats of the experimental group; 0.002 mg normal saline was injected into the rats of the control group through caudate nucleus; 0.002 mg morphine was injected into the rats of morphine group through caudate nucleus; 1.0 mg/kg naloxone was intraperitoneally into the rats of naloxone group, then 0.002 mg scorpion venom was injected into the rats of control group through caudate nucleus.Changes of evoked potential of PO of 3 groups were observed. ③After experiment, 1 μA direct current was given to the guiding electrode and micro electrode , and it lasted for 5 minutes. Pontamine sky blue was used to label the peak of electrode by electrophoresis. Brain tissue was soaked in formalin for 1 week then sliced into 1.0 to 1.5 mm sections. Electrode was orientated according to blue spots. Compared with G . Parino rat brain three-dimensional orientation atlas, we confirmed if the electrode orientation is consistent with PO orientation of G. Parino rat brain three-dimensional orientation atlas. MAIN OUTCOME MEASURES: Changes of the evoked potential of PO in each group. RESULTS: Totally 80 Wistar rats were enrolled in this experiment. Four rats in the experimental group and two in the morphine group died of overdose of anesthesia, and finally 74 rats entered the stage of result analysis. The inhibitory action time of evoked potential of PO has no statistical difference in between experiment group and morphine group (P > 0.05). The whole inhibitory action time, timeof initiate recovery and time of complete recovery of PO of experiment group were longer than those in the morphine group [(45±0.7),(50±9.2),(65±8.1);(35±7.8),(40±8.9),(50±7.6) min,P < 0.05].The change of evoked potential of PO was not obviously in the control group and naloxone group (P > 0.05), and the above-mentioned 4 indexes were nearly 0. CONCLUSION: Scorpion venom possesses obviously inhibitory effect on somatic pain, and its inhibitory effect is stronger than that of the same dosage and concentration of morphine. Scorpion venom exerts analgesic effect on somatic pain through opium acceptor.展开更多
We have reported that the central mechanism of acupuncture-induced PRL secretion in non-lactating rats are related to antagonizing hypothalamic dopamine activity; noradrenaline system played little significant role in...We have reported that the central mechanism of acupuncture-induced PRL secretion in non-lactating rats are related to antagonizing hypothalamic dopamine activity; noradrenaline system played little significant role in the acupuncture effect; Υ-aminobutyric-acid system perhaps participated in this effect.This paper further provided evidence that central serotonin and EOP play a stimulatory role in the acupuncture induced secretion of prolactin; acupuncture may antagonize inhibitory effect of H<sub>2</sub> histamine receptor activation on prolactin secretion; the possible role of H<sub>1</sub>-receptor needs further investigation.展开更多
Forty rots were randomized into 2 groups and naloxone or saline were injected to therats after they were inflicted with hemorrhagic shock at sea level and at a simulated altitude of4000m respectively to observe the ef...Forty rots were randomized into 2 groups and naloxone or saline were injected to therats after they were inflicted with hemorrhagic shock at sea level and at a simulated altitude of4000m respectively to observe the effects of naloxone on left ventricular systolic pressure(LVSP),left ventricular diastolic pressure(LVDP),the maximal changing rate of LVSP(dp/dt max),heartrate(HR),and survival time of the animals.Plasma β-endorphin(β-EP)was determined beforeand after hemorrhage to observe the relationship between β-EP and hemorrhagic shock.It wasfound that the circulatory parameters of hemorrhagic shock changed more markedly at high alti-tude than at sea level,naloxone could restore these parameters and prolong the survival time inboth the animals of the sea level and high altitude groups,and plasma β-EP level was elevatedafter hemorrhage especially in those animals at high altitude.These findings indicate:(1)Hemorrhagic shock at high altitude is usually accompanied with severe clinical manifestations,rapid progression,and high mortality.(2)β-EP seems to participate in the pathologicalmanifestafions of hemorrhagic shock at high altitude,and its depressive action on myocardialcontraction may be one of the factors inducing hemorrhagic shock.(3)Naloxone possesses defi-nite property to comet hemorrhagic shock at high altitude.展开更多
The increases of tracheal vascular permeability and malondialdehyde(MDA) content 1,2 and 3 h after introduction of hot air into the rat tracheaswere markedly inhibited by pethidine.The decreases of tracheal superoxide...The increases of tracheal vascular permeability and malondialdehyde(MDA) content 1,2 and 3 h after introduction of hot air into the rat tracheaswere markedly inhibited by pethidine.The decreases of tracheal superoxidedismutase (SOD) activity 2 and 3h after hot air injury were elevated bypethidine.However,the inhibitory effect of pethidine on tracheal vascularpermeability was not antagonized by naloxone.This implies that opiate receptorsensitive to naloxone is not involved in the inhibitory effect of pethidine ontracheal vascular permeability.Pethidine could decrease MDA content and in-crease SOD activity.These antioxidative effects are beneficial to decreasingvascular permeability.展开更多
We observed for the first time the differences of immunoreactive β-endorphin(IR -β- EP) content in plasma, pituitary and hypothalamus of rats under various conditionsusing radioimmunoassay (RIA) and the effects of n...We observed for the first time the differences of immunoreactive β-endorphin(IR -β- EP) content in plasma, pituitary and hypothalamus of rats under various conditionsusing radioimmunoassay (RIA) and the effects of naloxone and β - endorphin (β- EP) antiserumon initial time of convulsions (ITC), severity of convulsions(SOC) and mortality on surface(MOS) of rats to hyperbaric oxygen(HBO). The results suggest thatβ- EP may partici-pate in the course of oxygen - induced convulsions and be one of endogenous convulsion - causingagents.展开更多
文摘The opioid epidemic in the United States continues to take the lives of many individuals, with overdoses continuing to rise every year. Naloxone is an opioid antagonist that is efficacious in temporarily reversing opioid overdoses. Pharmacists play an important role in the accessibility and education of naloxone in both the community and health system settings. Recent efforts, such as co-dispensing naloxone with opioid prescriptions, naloxone training programs, and approval of naloxone to be over-the-counter, have been implemented in hopes to better control the opioid epidemic. Despite the efforts to make naloxone more accessible, there are still some barriers to overcome such as lack of training, cost, stigma, and patient refusal. This review aims to explore the contributions pharmacists have made thus far and define the barriers that still have to be resolved.
文摘Background: Controlled-release oxycodone/naloxone(OXN-CR) maintains the effect of opioid-induced analgesia through oxycodone while reducing the occurrence rate of opioid-induced constipation through naloxone. The present study was designed to assess the non-inferiority of OXN-CR to controlled-release oxycodone(OX-CR) for the control of cancer-related pain in Korean patients.Methods: In this randomized, open-labeled, parallel-group, phase IV study, we enrolled patients aged 20 years or older with moderate to severe cancer-related pain [numeric rating scale(NRS) pain score ≥4] from seven Korean oncology/hematology centers. Patients in the intention-to-treat(ITT) population were randomized(1:1) to OXNCR or OX-CR groups. OXN-CR was administered starting at 20 mg/10 mg per day and up-titrated to a maximum of80 mg/40 mg per day for 4 weeks, and OX-CR was administered starting at 20 mg/day and up-titrated to a maximum of 80 mg/day for 4 weeks.The primary efficacy endpoint was the change in NRS pain score from baseline to week4, with non-inferiority margin of-1.5. Secondary endpoints included analgesic rescue medication intake, patientreported change in bowel habits, laxative intake, quality of life(QoL), and safety assessments.Results: Of the ITT population comprising 128 patients, 7 with missing primary efficacy data and 4 who violated the eligibility criteria were excluded from the efficacy analysis. At week 4, the mean change in NRS pain scores was not significantly different between the OXN-CR group(n = 58) and the OX-CR group(n = 59)(-1.586 vs.-1.559,P = 0.948). The lower limit of the one-sided 95% confidence interval(-0.776 to 0.830) for the difference exceeded the non-inferiority margin(P < 0.001). The OXN-CR and OX-CR groups did not differ significantly in terms of analgesic rescue medication intake, change in bowel habits, laxative intake, QoL, and safety assessments.Conclusions: OXN-CR was non-inferior to OX-CR in terms of pain reduction after 4 weeks of treatment and had a similar safety profile. Studies in larger populations of Korean patients with cancer-related pain are needed to further investigate the effectiveness of OXN-CR for long-term pain control and constipation alleviation.Trial registration ClinicalTrials.gov NCT01313780, registered March 8。
文摘5-HT content in medulla oblongata plus pons and DA level in brain stem obviously increased,while NA concentration in telencephalon markedly decreased in EAA.A previous injection ofnaloxone,a blocker of opiate receptor,could partially inhibit the EAA,abolish the effects ofEA’s increasing the 5-HT content in the medulla oblongata plus pons and the DA level in thebrain stem,and decrease the NA level in the diencephalon after EA.These results indicate thatEA may mediate the metabolism of the central monoamine neurotransmitters partially via opiatereceptor to exert its analgesic effect.
文摘Stimulating SmI cortex like needling points produced analgesic effect in rats.Under the background of ventrical microinjecting atropine（10μg/2μl）or naloxone（20μg/20μl）tailflick latency（TEL）remained unchanged after stimulating SmI.Comparing atropine group or naloxone group with normal saline group it was shown that there were a statistical difference in TFL between the two groups respectively.Thus,both ACh and endogenous morphine-like factors may participate in analgesic effect as a neurotransmitter of the corticofugal modulation of pain.
文摘Objective: To investigate the effects of naloxone hydrochloride on pulmonary function, blood gas changes and inflammatory factors in patients with COPD combined with respiratory failure. Methods: According to random data table method, 80 cases of COPD combined with respiratory failure were randomly divided into the control group (n=40) and observation group (n=40), patients in the control group were treated with noninvasive positive pressure ventilation on the basis of routine symptomatic treatment, on the basis of the treatment of the control group, the observation group received naloxone hydrochloride therapy. The levels of pulmonary function, blood gas changes and inflammatory factors were compared in two groups before and after treatment. Results: The levels of serum FEV1, FVC, PEF, PaCO2, PaO2, PaO2/FiO2, TNF-α and PCT in the two groups before treatment were not statistically significant. After treatment, the levels of FEV1, FVC, PEF in the control group and observation group were (70.01±0.36)%, (2.16±0.41) L, (2.98±0.45) L/s and (81.71±0.53)%, (3.65±0.55) L, (4.36±0.43) L/s, which were significantly higher than those in the same group before treatment, and the levels in observation group were significantly higher than those in the control group;the levels of PaCO2, PaO2 and PaO22/FiO2 in the two groups were (59.62±6.47) mmHg, (65.53±7.36) mmHg, (323.89±10.47) and (46.59±6.64) mmHg, (73.65±8.26) mmHg, (398.64±14.06), compared with the same group before treatment, PaCO2 levels were significantly lower in both groups, and the observation group was significantly lower than the control group, PaO2,PaO2/FiO2 levels were significantly increased in both groups, and the observation group was significantly higher than the control group;the levels of TNF-α, PCT in the two groups were (23.28±4.53) pg/mL, (5.22±2.13) ng/mL and (16.61±4.12) pg/mL, (2.07±1.21) ng/mL, which were significantly lower than those in the same group before treatment, moreover, the observation group levels were significantly lower than those in the control group. Conclusion:Treatment of COPD with respiratory failure by naloxone hydrochloride can effectively reduce the level of inflammatory factors, and improved lung function and blood gas levels, which has important clinical value.
文摘Objective: To investigate the effect of Shenqi Fuzheng Injection combined with naloxone and BiPAP ventilator on serum inflammatory factors, immune function and blood gas analysis indexes in treatment of AECOPD with type Ⅱ respiratory failure. Methods: A total of 82 patients with AECOPD and type Ⅱ respiratory failure were divided into control group (n=40) and observation group (n=42) according to random data table, patients in the control group received naloxone and BiPAP ventilator therapy, and observation group patients were treated with Shenqi Fuzheng Injection on the basis of control group. The levels of serum inflammatory factors, immune function and blood gas analysis indexes were compared between the two groups before and after treatment. Results: There were no significant difference in levels of CRP, TNF-α, IL-6, CD3+, CD4+, CD8+, CD4+/CD8+, PaO2, PaCO2, SaO2 and pH before and after treatment in the two groups. After treatment, the levels of CRP, TNF-α, IL-6, CD8+and PaCO2 in two groups were significantly lower than those in same group before treatment, moreover observation group was significantly lower than control group;and levels of CRP, TNF-α, IL-6, CD8+ and PaCO2 in the observation group was significantly lower than those of the control group, the difference was statistically significant;When compared with the group before treatment, CD3+, CD4+, CD4+/CD8+, PaO2, SaO2 and pH levels of both groups after treatment were significantly increased, and the level of each index of observation group after treatment were significantly higher than the control group, the difference was statistically significant. Conclusion: The clinical effect of Shenqi Fuzheng Injection Combined with naloxone and BiPAP ventilator in treatment of AECOPD with type II respiratory failure is significant, can effectively reduce the body's inflammatory reaction, improve immune function, regulate blood gas analysis index, with a certain clinical value.
基金supported by a grant from the Deputy of Research and Technology,Health Ministry of Iran[Grant no.642]partially by a grant from the Pasteur Institute of Iran。
文摘Objective This study aimed to investigate the effects of Montanide ISA-720 and Naloxone(NLX)in Hepatitis B surface antigen(HBsAg)vaccine formulation on cytokine and long-lasting antibody responses.Methods First,the HBsAg was formulated in Montanide ISA-720 adjuvant and Naloxone at 5 and 10mg/kg.The experimental mice were immunized three times at a 2-week interval,and then IL-4,IL-2,TNF-α,and IFN-γcytokines;long-lasting IgG antibody responses 220 days after the last shot;and IgG1/IgG2a isotypes were assessed by ELISA.Results The HBsAg-Alum group exhibited the highest IL-4 cytokine response among the experimental groups,whereas NLX in HBsAg-MON720 vaccine formulation did not affect cytokine responses.In addition,NLX in Alum-based vaccine suppressed IL-4 cytokine response and increased the IL-2/IL-4 cytokine ratio.Moreover,HBsAg-MON720 was more potent than HBsAg-Alum in the induction of antibody responses,and NLX in Alum-and MON720-based vaccines induced long-lasting antibody responses.Conclusion NLX in Alum-based vaccine decreased IL-4 cytokine response,increased IL-2/IL-4 cytokine ratio,and improved long-lasting humoral immune responses in both vaccine formulations.Therefore,the adjuvant activity of NLX in the vaccine formulation depends on the type of adjuvant and the nature of the antigen in the vaccine formulation.
基金the financial support received from the Natural Science Foundation of Liaoning Province [No. 20180550155, 2021-MS-332]the National Natural Science Foundation of China (No.81671907, 81871556, 82072165)+2 种基金LiaoNing Revitalization Talents Program (No. XLYC1902108)Scientific Research Project of the Educational Department of Liaoning Province(No. JYTQN201917, JYTQN201919)Liaoning Provincial Key Laboratory of Marine Bioactive Substances and Technological Innovation Center of Liaoning Pharmaceutical Action and Quality Evaluation (No. 2020–10)。
文摘Spinal cord injury(SCI)causes Ca^(2+) overload,which can lead to inflammation and neuronal apoptosis.In this study,we prepared a nanovesicle derived from macrophage membrane(MVs),which encapsulated sodium alginate(SA)and naloxone(NAL)to inhibit inflammation and protect neurons by reducing the free Ca^(2+) concentration at the SCI site.Based on the transmission electron microscopy(TEM)image,the encapsulated sample(NAL–SA–MVs)had a particle size of approximately 134±11 nm and exhibited a sustained release effect.The encapsulation rate of NAL and SA was 82.07%±3.27%and 72.13%±2.61%in NAL–SA–MVs,respectively.Targeting tests showed that the NAL–SA–MVs could accumulate in large quantities and enhance the concentration of SA and NAL at the lesion sites.In vivo and in vitro studies indicated that the NAL–SA–MVs could decrease the concentration of free Ca^(2+),which should further alleviate the inflammatory response and neuronal apoptosis.Anti-inflammation results demonstrated that the NAL–SA–MVs could reduce the pro-inflammation factors(iNOS,TNF-α,IL-1β,IL-6)and increase the expression of antiinflammation factors(IL-10)at the cell and animal level.Concurrently,fluorescence,flow cytometry and western blot characterization showed that the apoptotic condition of the neurons was significantly inhibited.In addition,the motor function of C57 mice were significantly improved after NAL–SA–MVs treatment.In conclusion,it is suggested that the NAL–SA–MVs has tremendous potential in the treatment of SCI.
文摘Experiments were performed on SD rats. The animals were anesthetized with urethane (1. 0 g/kg, i. p. ). The diaphragmatic electric activity and intratracheal pressure were monitored. Morphine (4 mg/kg, i. v. ) caused marked respiratory inhibition. The respiratory frequency (RF), integrated diaphragmatic electric activity (IDEA) and diaphragmatic minute activity (DMA) were decreased. The respiratory depression effect of morphine was almost completely eliminated by pretreatment with naloxone injected into the medial areas of the nucleus retrofacialis (mNRF). Bilateral microinjection of morphine (5 μg) into mNRF might result in apnea in all animals. This effect could be fully prevented by injection of naloxone into mNRF in advance. The results suggest that there might be morphine receptors in the mNRF and they might play an important role in the respiratory inhibition induced by systemic administration of morphine.
文摘The recent large increase in deaths involving opioids (whether prescription or illicit, pure or adulterated, alone or in combination with other drugs) is the manifestation of a complex, and multifaceted problem consisting of psychological, psychosocial, medical, legal, regulatory, economic, cultural, and political components, among others. Because the problem involves issues related to both supply and demand, the solution is not obvious, simple, or quick. There is no easy fix. Preventing and treating opioid misuse and abuse requires a comprehensive, time-intensive, and expensive intervention supported by public policy and support through coordinated medical, regulatory, legal, and financial guidelines and practice. But until the long-term problems can be fixed, the immediate crisis of overdose deaths can be ameliorated by making available an opioid receptor antagonist to reverse the respiratory depression that is the cause of death to those who are in the best position to administer it in time (professionals, untrained bystanders, and even fellow drug abusers). The statistics overwhelmingly demonstrate that this is a life-saving medical intervention. Yet, there is still uncertainty about this intervention, and even some opposition to it. We describe the scientific basis for the approach and the issues surrounding its use to treat accidental or intentional overdose by pain patients, recreational opioid users, and addicts. We also describe the calls to limit the number of times it should be available to a user and the limitations of its effectiveness—mainly that it only addresses the acute death crisis, not the underlying problems that led to it.
文摘The mechanism(s) of analgesic action of paracetamol (acetaminophen;N-acetyl-p-aminophenol) remains controversial. Previous studies on rats suggested that the antinociceptive action of paracetamol might involve the central descending inhibitory pain pathways recruiting both a serotoninergic and an opioidergic system. This study explores this issue in mice using paroxetine, the most potent selective serotonin re-uptake inhibitor, and the nonselective opioid pure antagonist naloxone. Animals were divided into two main groups for two separate experiments, each subdivided into 3 subgroups. In both experiments;the first group served as control, the second group received paracetamol (200 mg/kg, i.p). In one experiment, the third group received paroxetine (20 mg/kg p.o for 7 days) before paracetamol. In the other experiment, animals of the third group were pretreated with naloxone (5 mg/kg, i.p) 30 min before paracetamol. The antinociceptive effect of paracetamol was tested using the hot plate test. Paracetamol displayed a significant antinociceptive activity that was augmented by pretreatment with paroxetine as was shown by maintenance of its effect beyond that shown by paracetamol alone. On the other hand, pretreatment with naloxone abolished paracetamol’s antinociceptive activity in the hot-plate test. These results extended the previous observation in rats that the antinociceptive effect of paracetamol involved activation of a central descending pain inhibitory pathway with serotonin and opioidergic peptides being potential mediators recruited.
文摘A 56-year-old man presented to the emergency department after an intentional overdose of oxycodone and ethanol.He was previously opioid-naive with no other medical history.He subsequently developed acute abdominal pain with nausea and vomiting.A computed tomography scan of his abdomen and pelvis revealed distension of his stomach with no other abnormalities suggestive gastroparesis.He was subsequently treated with intravenous naloxone with complete resolution of his symptoms soon after.This case highlights the association between opioids and acute gastrointestinal mobility disorders contrary to the traditional association with chronic opioid use,as well as the utility of naloxone as a treatment.
基金Supported by the National Natural Science Foundation of China(No.81473547,81673829)the Beijing Municipal Organization Department Talents Project(No.2017000020124G292)
文摘Objectives:To investigate the effectiveness and safety of Xingnaojing Injection(XNJ,醒脑静注射液)compared with naloxone for the treatment of acute alcohol intoxication(AAI),and provide the latest evidence through evidence-based approach.Methods:Seven electro-databases including Pub Med,EMBASE,Cochrane Central Register of Controlled Trials,Chinese National Knowledge Infrastructure Databases,Chinese Biomedical Literature Database,Chinese Science and Technology Periodical Database(VIP)and Wanfang Database were searched from the inception to January 2018.Randomized controlled trials(RCTs)comparing XNJ with naloxone for patients with AAI and reporting at least one of the below outcomes were included:patients’conscious recovery time,stay length in emergency department,disappearance time of the ataxia symptom,the severity of the symptoms,the blood alcohol content as wel as the adverse events.Methodological quality of included trials was assessed using the risk of bias tool which recommended by the Cochrane Col aboration.Meta-analysis was conducted by Review Manager 5.3 software.Results:Total y 141 trials with 13,901 patients were included in this review,al of them were assessed as unclear or high risk of bias.Results showed that on the basis of routine therapy,standard dose XNJ(10–20 m L)may have similar results with naloxone on the recovery time of consciousness(MD 12 min,95%CI 7.2–17.4 min)and disappearance time of symptoms(MD 6 min,95%CI–13.8–25.8 min)for patients with AAI.Larger dose of XNJ Injection(21–40 m L)may speed up the time(almost 1 h earlier).Combination of XNJ and naloxone seemed superior to the naloxone alone for al the relevant outcomes.The average difference of time in consciousness recovery was 2 h and the number of AAI patients whose consciousness recovery within 1 h was above 50%the combination group than in the control group(RR 1.42,95%CI 1.29 to 1.56).No severe adverse events or adverse reactions of XNJ were reported in the included trials.Conclusions:Low quality of evidence showed XNJ may have equal effect as naloxone and may achieve better effect as add-on intervention with naloxone for patients with AAI.We failed to evaluate the safety of XNJ Injection due to the insufficient evidence in this review.
基金This wark was supported by the grant from the Scientific Fund of Academia Sinica (82, No.100)
文摘It has been shown in our previous experiments that arcuate nucleus (ARC) stimulation had a marked analgesic effect. After selective lesion of ARC neurons by neonatally intrapcritoneal injection of monosodium glutamate (MSG), the analgesic effects of morphine, acupuncture and stress decreased significantly.
文摘BACKGROUND: Scorpion venom from Buthus martensii Karsch is a kind of protein toxin secreted by scorpion tail. According to records of Pen-ts’ao Kan-mu, the dried scorpion’s body and tail are used as medicine, which mainly treating rheumatism numbness, pain and convulsion. Some researches consider that scorpion toxin is the main pharmacological active component of the dried scorpion, and it has 4 times stronger analgesic effect on somatic pain than morphine. OBJECTIVE: To observe the interventional effect of scorpion venom of Buthus martensii Karsch analgesic active peptide on somatic pain. DESIGN: A randomized and controlled trial. SETTING: Department of Physiology, Shenyang Medical College. MATERIALS: Totally 80 Wistar rats (provided by Animal Center of Shenyang Medical College), male and female in half, aged 3 to 4 months, weighed 250 to 350 g, were used in this trial. They were randomly divided into 4 groups: experimental group, control group, morphine group and naloxone group, with 20 in each group. Analgesia active peptide from buthus martensii karsch venom (provided by Biochemical Department of Shenyang Pharmaceutical University, 1 mL/dosage), morphine (produced by Shanghai First Pharmaceutical Manufacturing Plant), naloxone (opium acceptor inhibitor, American Sigma Corporation), ATAC-350 data-processing machine (Nihon Kohden Corporation), X-Y recording instrument (Nihon Kohden Corporation). METHODS: The experiment was conducted in the Department of Physiology, Shenyang Medical College from July 2003 to July 2005. ① After all the animals were anesthetized, common peroneal nerve is dissected and ligated at middle part. Posterior nucleus group of thalamus (PO) and the tail nuclear were oriented according to G. Paxino rat brain three-dimensional orientation atlas. Glass micro electrode was inserted into PO as guiding electrode, connected with ATAC-350 data-processing machine and X-Y recording instrument, to record the unit evoked potential of PO, taking the evoked potential discharge of the common peroneal nerve of PO as the somatic pain index.② Single square-wave stimulation of intensity 17-19 volt, wave wide 0.2 ms, time delay 20 ms was exerted on common peroneal nerve. The time interval was 5 minutes. X-Y recording instrument was used to draw the graph. 0.002 mg scorpion venom analgesic active peptide was injected into the rats of the experimental group; 0.002 mg normal saline was injected into the rats of the control group through caudate nucleus; 0.002 mg morphine was injected into the rats of morphine group through caudate nucleus; 1.0 mg/kg naloxone was intraperitoneally into the rats of naloxone group, then 0.002 mg scorpion venom was injected into the rats of control group through caudate nucleus.Changes of evoked potential of PO of 3 groups were observed. ③After experiment, 1 μA direct current was given to the guiding electrode and micro electrode , and it lasted for 5 minutes. Pontamine sky blue was used to label the peak of electrode by electrophoresis. Brain tissue was soaked in formalin for 1 week then sliced into 1.0 to 1.5 mm sections. Electrode was orientated according to blue spots. Compared with G . Parino rat brain three-dimensional orientation atlas, we confirmed if the electrode orientation is consistent with PO orientation of G. Parino rat brain three-dimensional orientation atlas. MAIN OUTCOME MEASURES: Changes of the evoked potential of PO in each group. RESULTS: Totally 80 Wistar rats were enrolled in this experiment. Four rats in the experimental group and two in the morphine group died of overdose of anesthesia, and finally 74 rats entered the stage of result analysis. The inhibitory action time of evoked potential of PO has no statistical difference in between experiment group and morphine group (P > 0.05). The whole inhibitory action time, timeof initiate recovery and time of complete recovery of PO of experiment group were longer than those in the morphine group [(45±0.7),(50±9.2),(65±8.1);(35±7.8),(40±8.9),(50±7.6) min,P < 0.05].The change of evoked potential of PO was not obviously in the control group and naloxone group (P > 0.05), and the above-mentioned 4 indexes were nearly 0. CONCLUSION: Scorpion venom possesses obviously inhibitory effect on somatic pain, and its inhibitory effect is stronger than that of the same dosage and concentration of morphine. Scorpion venom exerts analgesic effect on somatic pain through opium acceptor.
基金Project supported by the National Natural Science Fund
文摘We have reported that the central mechanism of acupuncture-induced PRL secretion in non-lactating rats are related to antagonizing hypothalamic dopamine activity; noradrenaline system played little significant role in the acupuncture effect; Υ-aminobutyric-acid system perhaps participated in this effect.This paper further provided evidence that central serotonin and EOP play a stimulatory role in the acupuncture induced secretion of prolactin; acupuncture may antagonize inhibitory effect of H<sub>2</sub> histamine receptor activation on prolactin secretion; the possible role of H<sub>1</sub>-receptor needs further investigation.
文摘Forty rots were randomized into 2 groups and naloxone or saline were injected to therats after they were inflicted with hemorrhagic shock at sea level and at a simulated altitude of4000m respectively to observe the effects of naloxone on left ventricular systolic pressure(LVSP),left ventricular diastolic pressure(LVDP),the maximal changing rate of LVSP(dp/dt max),heartrate(HR),and survival time of the animals.Plasma β-endorphin(β-EP)was determined beforeand after hemorrhage to observe the relationship between β-EP and hemorrhagic shock.It wasfound that the circulatory parameters of hemorrhagic shock changed more markedly at high alti-tude than at sea level,naloxone could restore these parameters and prolong the survival time inboth the animals of the sea level and high altitude groups,and plasma β-EP level was elevatedafter hemorrhage especially in those animals at high altitude.These findings indicate:(1)Hemorrhagic shock at high altitude is usually accompanied with severe clinical manifestations,rapid progression,and high mortality.(2)β-EP seems to participate in the pathologicalmanifestafions of hemorrhagic shock at high altitude,and its depressive action on myocardialcontraction may be one of the factors inducing hemorrhagic shock.(3)Naloxone possesses defi-nite property to comet hemorrhagic shock at high altitude.
文摘The increases of tracheal vascular permeability and malondialdehyde(MDA) content 1,2 and 3 h after introduction of hot air into the rat tracheaswere markedly inhibited by pethidine.The decreases of tracheal superoxidedismutase (SOD) activity 2 and 3h after hot air injury were elevated bypethidine.However,the inhibitory effect of pethidine on tracheal vascularpermeability was not antagonized by naloxone.This implies that opiate receptorsensitive to naloxone is not involved in the inhibitory effect of pethidine ontracheal vascular permeability.Pethidine could decrease MDA content and in-crease SOD activity.These antioxidative effects are beneficial to decreasingvascular permeability.
文摘We observed for the first time the differences of immunoreactive β-endorphin(IR -β- EP) content in plasma, pituitary and hypothalamus of rats under various conditionsusing radioimmunoassay (RIA) and the effects of naloxone and β - endorphin (β- EP) antiserumon initial time of convulsions (ITC), severity of convulsions(SOC) and mortality on surface(MOS) of rats to hyperbaric oxygen(HBO). The results suggest thatβ- EP may partici-pate in the course of oxygen - induced convulsions and be one of endogenous convulsion - causingagents.
